1. MAPK/ERK Pathway
  2. p38 MAPK
  3. (R)-STU104

(R)-STU104 

Cat. No.: HY-150612
Handling Instructions

(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis.

For research use only. We do not sell to patients.

(R)-STU104 Chemical Structure

(R)-STU104 Chemical Structure

CAS No. : 2767124-77-4

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Description

(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis[1].

IC50 & Target

IC50: 0.58 μM (TNF-α), 4.0 μM (MKK3 phosphorylation)[1]

In Vitro

(R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

(R)-STU104 (1, 3 and 10 mg/kg; IG for 7 days) ameliorates the symptoms of DSS-induced experimental colitis in mice, and significantly inhibits inflammatory cytokine protein[1].
Pharmacokinetic Parameters of (R)-STU104 in male C57 mice[1].

IV (5 mg/kg) PO (30 mg/kg)
Tmax (h) 0.083
AUC0-t (μg/L·h) 7249 9895
AUC0-∞ (μg/L·h) 8635 16991
MRT0-∞ (h) 7.32 12.52
Cmax (ng/mL) 2920 2290
t1/2 (ng/mL) 9.29 8.67
VZ (L/kg) 7.76 3.68
CLZ (ng/mL) 0.58 0.29
F (%) 33%

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (dextran sodium sulfate (DSS)-induced acute ulcerative colitis)[1]
Dosage: 1, 3 and 10 mg/kg
Administration: IG, for 7 days
Result: Ameliorated the symptoms of DSS-induced experimental colitis, and significantly inhibited inflammatory cytokine protein TNF-α, IL-1β, IL-6, and IL-23.
Molecular Weight

298.33

Formula

C18H18O4

CAS No.
SMILES

O=C1C[[email protected]](C2=CC=C(OC)C=C2)C3=C1C=C(OC)C=C3OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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(R)-STU104
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HY-150612
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